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Prasugrel hydrochloride is a novel antiplatelet agent that is a third-generation thienopyridine. Prasugrel produces inhibition of platelet aggregation to 20 μM or 5 μM ADP. Prasugrel hydrochloride binds to P2Y12 receptors and showed greater platelet inhibition and decreased incidence of ischemic events when compared to clopidogrel. In the absence of lansoprazole, the extent of absorption (AUC) of prasugrel free base was about 8-9% lower, while the rate of absorption (Cmax) after administration of prasugrel free base was 20% lower when compared to prasugrel hydrochloride. When lansoprazole was used to raise the pH level in the upper gastro-intestinal tract, AUC was decreased by 25% after administration of prasugrel hydrochloride and by 41% after prasugrel free base. In addition, the peak plasma levels were decreased by 52% and 72%, respectively (geometric means). The relative bioavailability of the prasugrel free base compared to prasugrel hydrochloride, both in the presence and in the absence of the proton pump inhibitor lansoprazole, differs so much that most probably a generic formulation containing prasugrel free base will not be equivalent in all aspects to the originator product.
| Molecular Weight | 409.91 |
| Formula | C20H20FNO3S.HCl |
| CAS Number | 389574-19-0 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related P2 Receptor Products |
|---|
| GW 791343 dihydrochloride
GW 791343 dihydrochloride is a non-competitive inhibitor of human P2X(7) receptor. |
| Prasugrel
Prasugrel is a platelet inhibitor irreversibly binding to P2Y12 receptors. |
| MRS 2578
MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
| PPADS Tetrasodium
PPADS tetrasodium salt is a non-selective P2 purinergic antagonist blocking recombinant P2X1, P2X2, P2X3, P2X5 with IC50 of 1-2.6 μM, native P2Y2-like with IC50 of ~ 0.9 mM, and recombinant P2Y4 receptors with IC50 of ~ 15 mM |
| Ticagrelor
Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM respectively. |
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